Study your flashcards anywhere!

Download the official Cram app for free >

  • Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/117

Click to flip

117 Cards in this Set

  • Front
  • Back
Atropine
deadly nightshade
Digoxin
foxglove
Morphine
sap from poppy plant
Quinine
bark of cinchona tree
Paclitaxel
bark of Western yew tree
Cocaine
coca shrub leaves
Insulin
beef or pork pancreas
Heparin
porcine intestinal mucosa
bovine lung
Abciximab
Monoclonal antibodies
Used in coronary bypass to prevent blood from clotting
Monoclonal antibody drug used for rheumatoid arthritis
Infliximab
Trastuzumab
breast cancer treatment
-olol
beta-adrenergic antagonist
local anesthetic
-caine
-dipine
calcium channel antagonist of dihydropyridine type
histamine-2 receptor antagonist
-prazole
-zosin
alpha-1 receptor antagonist
ACE inhibitors
-pril
1906 Federal Pure Food & Drug Act
standards for strength & purity but does not check for safety
1938 Federal Food, Drug, & Cosmetic Act
requires testing for safety before marketing
1962 Harris-Kefauver Amendment
required proof of efficacy & safety before marketing and the FDA has to be notified before testing on humans
1970 Comprehensive Drug Abuse & Prevention Control Act
controls for manufacturers & prescribers of habit-forming drugs
1983 Orphan Drug Act
establishes programs & incentives for development of drugs to treat rare diseases
1984 Drug Price & Patent Resoration Act
required new drug applications for generic drug products
Time frame for early research & preclinical testing
6.5 years
What does early research & preclinical testing assess?
safety & biological activity
What has to be done first before Phase 1 can begin?
File an IND (investigational new drug) application with the FDA
What does Phase 1 determine?
safety & dosage
How much time is required for Phase 1?
1 year
How much time is required for Phase 2?
2 years
What does Phase 2 evalulate?
effectiveness, look for side effects
How much time is required for Phase 3?
3.5 years
What does Phase 3 do?
effectiveness & monitors adverse reactions from long term use
What has to be done for pre-marketing approval?
Need to file a NDA (new drug application) with the FDA which takes 1.5 years
Describe the 5 categories of labeling for use in pregnant women
A--controlled studies showing no risk

B--no risk in animal studies, no human studies done

C--adverse fetal effects in animals, use only if benefit outweighs risk

D--demonstrate human fetal risk, may use despite risk

X--risk outweighs any possible benefit
What is an example of a Category X drug?
Acutane
FDA Modernization Act of 1997
provides incentives, mainly patent extension, for clinical pharmacology in children
Pediatric Rule of 1998
studies must be done unless valid reasons not to do so
Describe 5 categories of controlled substances & give examples of each
1--no accepted medical use
(heroin, LSD)

2--high abuse potential
(morphine, cocaine,
amphetamines)

3--less abuse potential
(codeine + acetaminophen,
hydrocodone)

4--diazepam

5--codeine-containing cough
syrups, pseudoephedrine
Describe filtration/aqueous diffusion
small pores in membrane or gaps between cells, drugs are often too big to pass through
Describe passive diffusion
lipid soluble, unbound, and non-ionized drugs dissolve in membrane
What is the driving force for passive diffusion?
concentration gradient
Properties that influence rate & extent of transport by passive diffusion
-size of drug
-degree of ionization
-lipid solubility
-concentration gradient
-surface area for diffusion
What is equilibrium partition coefficient?
-measure of lipophilicity
-amount dissolved in oil/water
What determines ionization?
pKa of drug & pH of medium
Is aspirin a weak acid or base?
weak acid
What are weak acids?
chemicals which can form salts
In what pH do weak acids better dissolve?
low pH
What are weak bases?
chemicals that form salts with acids
In what pH do weak bases better dissolve?
high pH
What is ion trapping?
weak acidic or basic drugs may concentrate to one side of the membrane when the pH of fluids on either side are different
What is facilitated diffusion?
carrier-mediated process carrying some chemicals across the membrane such as glucose and amino acids
What is the driving force for facilitated diffusion?
concentration gradient
Is facilitated diffusion saturable?
Yes
What is active transport?
requires chemical energy to drive the transport
Does active transport depend on concentration gradient?
transports against a concentration gradient
Describe the multiple drug resistant P-glycoprotein
-anti-cancer drug enters cell via passive diffusion
-when cells develop resistance, P-glycoprotein carrier pumps out the drug
-concentration cannot build up in the cell
What is bioavailability?
fraction the dose of the drug that reaches the systemic circulation
What does the rate & extent of absorption depend on?
-blood flow to the site of administration
-surface area of diffusion
-ionization state of the drug
-lipophilicity of the drug
What is the most important & commonly used route of administration?
oral
What are the 10 different routes of administration?
-oral
-sublingual
-rectal
-intravenous
-subcutaneous
-intramuscular
-inhalation
-intraperitoneal
-intrathecal
-topical
What is the first pass effect?
removal of significant portion of a drug dose by metabolism during the first pass of the drug through the GI mucosa & liver, only fraction of the oral dose reaches peripheral circulation
What does intrathecal mean?
entry of drug into CNS (spinal anesthesia)
What properties of oral mucosa favor absorption?
thin epithelium, rich vascularity
What property of oral mucosa do not favor absorption?
small surface area
What factors influence absorption from the stomach?
-properties of the drug (degree of ionization, lipophilicity, molecular weight, solubility in aqueous GI fluids, stability in acid & digestive enzymes)
-binding of drug to food particles
-surface area
-blood flow
-gastric emptying time
What is a main feature of the small intestine to help with absorption?
largest GI surface area
What are some properties of the small intestine that affect absorption?
-surface area
-pH environment variation (more acidic in duodenum than ileum)
-GI flora may inactivate certain drugs
-drug transit slow
What are the factors that influence absorption in the small intestine?
-properties of the drug (degree of ionization, lipophilicity, molecular weight, susceptibility to digestive enzymes & GI flora, solubility in aqueous GI fluids)
-binding of drug to food particles
-surface area
-blood flow
Describe how L-Dopa is absorbed?
-NOT by passive diffusion
-carried across by same carrier that carries phenylalanine
What compounds besides L-Dopa are not absorbed by passive diffusion?
toxic compounds such as lead & the herbicide paraquat
What is a big difference between large and small intestine that affects absorption?
no villi
What are 2 different routes of drug once it enters the gut lumen?
1--goes right through liver & into systemic circulation
2--metabolized in liver
What are some ways to increase the amount of drug found in the peripheral circulation?
-administer via IV
-increase drug
-change drug
What are 4 reasons why most drugs are administered orally in tablets or capsules?
-convenience
-economy
-stability
-patient acceptance
Why are drug tablets designed to dissociate?
increases drug surface area
How can you reduce the dissolution of drugs into GI fluids?
coating particles with wax or other water-insoluble material & embedding drug into a matrix
What is parenteral?
-direct placement of drug into the blood stream to ensure bioavailability
-still has to penetrate through membranes
What determines the rate of entry into capillaries?
-hydrophobicity of drug
-rate of capillary blood flow
How can you slow absorption of local anesthetic drugs injected SQ for local pain relief?
administer vasoconstrictors (epi), heat or cold
What happens when salts of poorly soluble acids & bases are injected IM?
absorption may be delayed or erratic
Describe what happens with phenytoin (an anti-convulsant)
-water soluble only as the Na salt in a solution with a pH of ~12
-injected IM -> tissue fluids act as buffers & pH decreases -> shift to produce more free acid (HA), which precipitates at the site of injection & absorbs very slowly
What are some advantaes of prolonged release dosage forms of drugs?
-reduce frequency of dosing
-can maintain more uniform plasma drug concentration
-may improve drug compliance
Describe the procaine salt of penicillin
-poorly soluble, slowly absorbed
-prolonged by suspending penicillin in oil containing aluminum stearate
-oil prevents contact of salt with aqueous medium, retarding dissolution
-aluminum stearate further delays dissolution by increasing viscosity
About how much total body water is in a 70 kg person? How much of that is plasma? Interstitial fluid? Intracellular fluid? Extracellular fluid?
-60% of ody weight, 42 liters
-Plasma: 4%, 3 liters
-Interstitial Fluid: 16%, 11 liters
-Intracellular Fluid: 40%, 28 liters
-Extracellular Fluid: 20%, 14 liters
Which are more permeable--cell membranes or capillary walls?
Capillary walls because they have large pores allowing ultrafiltration of smaller molecules to take place
What is the primary plasma binding protein?
albumin
What is the function of plasma binding proteins?
-keeps concentration of free drug in plasma low
-enhances drug absorption since the rate of absorption by non-ionic diffusion is proportional to the concentration gradient of free drug from the site of administration into the blood stream
-if drug is actively transported, movement across membranes is NOT reduced
What happens with people that have hypoalbuminemia?
-more free drug is in plasma -> enhanced absorption to concentration level that is toxic
What are the 3 things that characterize plasma protein binding?
-Reversibility
-Saturation
-Competition
Describe reversibility
-free drug leaves circulation, remaining complexes dissociate -> release more free drug for diffusion
-protein-bound drug may be depot
Describe saturation
plasma concentration increases -> available protein binding sites decreases
What kinds of drugs are able to distribute to the CNS?
highly lipid soluble drugs, due to BBB
What factors of the CNS limit diffusion?
-endothelial cells of capillaries much more firmly joined
-capillaries sheathed with processes of astrocytes
What are some things that can increase the permeability of the BBB?
-infants
-inflammation
Describe the distribution through the placenta
-placenta is rather permeable
-there is a time lag between drug concentration in maternal blood & that in fetal blood
-rate of maternal blood limits availability of drug to fetus
-placenta slow drug movement, but does not prevent distribution
What determines differential distribution?
-binding of drugs to plasma proteins or tissue
-storage of drugs by body fat, BBB
-active transport in the liver, kidney, & other organs
Describe saturation
plasma concentration increases -> available protein binding sites decreases
Describe saturation
plasma concentration increases -> available protein binding sites decreases
What are targeted drug?
drugs designed to achieve high concentrations at the site of action
What kinds of drugs are able to distribute to the CNS?
highly lipid soluble drugs, due to BBB
What kinds of drugs are able to distribute to the CNS?
highly lipid soluble drugs, due to BBB
What is redistribution of drugs and what is a good example?
-initial distribution of drugs often follows distribution of blood flow, then drug redistribute according to affinity
-example: thiopental -> first goes to brain & later redistributes to adipose tissue & muscle (lower blood flow)
What factors of the CNS limit diffusion?
-endothelial cells of capillaries much more firmly joined
-capillaries sheathed with processes of astrocytes
What factors of the CNS limit diffusion?
-endothelial cells of capillaries much more firmly joined
-capillaries sheathed with processes of astrocytes
What are some things that can increase the permeability of the BBB?
-infants
-inflammation
What is the volume of distribution (Vd)?
-volume of fluid needed to maintain a drug in the same concentration as in the plasma
-Vd = A / CPo
-A=amount of drug in body
-CPo=plasma concentration of the drug following distribution of the drug to tissues & before elimination of the drug occurs
What are some things that can increase the permeability of the BBB?
-infants
-inflammation
Describe the distribution through the placenta
-placenta is rather permeable
-there is a time lag between drug concentration in maternal blood & that in fetal blood
-rate of maternal blood limits availability of drug to fetus
-placenta slow drug movement, but does not prevent distribution
What determines differential distribution?
-binding of drugs to plasma proteins or tissue
-storage of drugs by body fat, BBB
-active transport in the liver, kidney, & other organs
Describe the distribution through the placenta
-placenta is rather permeable
-there is a time lag between drug concentration in maternal blood & that in fetal blood
-rate of maternal blood limits availability of drug to fetus
-placenta slow drug movement, but does not prevent distribution
What determines differential distribution?
-binding of drugs to plasma proteins or tissue
-storage of drugs by body fat, BBB
-active transport in the liver, kidney, & other organs
What are targeted drug?
drugs designed to achieve high concentrations at the site of action
What are targeted drug?
drugs designed to achieve high concentrations at the site of action
What is redistribution of drugs and what is a good example?
-initial distribution of drugs often follows distribution of blood flow, then drug redistribute according to affinity
-example: thiopental -> first goes to brain & later redistributes to adipose tissue & muscle (lower blood flow)
What is redistribution of drugs and what is a good example?
-initial distribution of drugs often follows distribution of blood flow, then drug redistribute according to affinity
-example: thiopental -> first goes to brain & later redistributes to adipose tissue & muscle (lower blood flow)
What is the volume of distribution (Vd)?
-volume of fluid needed to maintain a drug in the same concentration as in the plasma
-Vd = A / CPo
-A=amount of drug in body
-CPo=plasma concentration of the drug following distribution of the drug to tissues & before elimination of the drug occurs
What is the volume of distribution (Vd)?
-volume of fluid needed to maintain a drug in the same concentration as in the plasma
-Vd = A / CPo
-A=amount of drug in body
-CPo=plasma concentration of the drug following distribution of the drug to tissues & before elimination of the drug occurs